JTT-851 (CAS: )
Background Information of JTT-851
JTT-851 is a GPR40 partial agonist. GPR40, also known as FFAR1, belongs to the class A family of G-protein coupled receptors, and is expressed predominantly in pancreatic β cells and enteroendocrine cells.GPR40 partial agonism is a promising new mechanism for the treatment of type 2 diabetes mellitus with clinical proof of concept.
Storage Condition of JTT-851
Quality Control and Spectral Data
Mechanism and Indications
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Structure Information of JTT-851
||C1CCC2(CC(COC3C=CC([[email protected]](C(O)=O)C#CC)=CC=3)=CCC2)CC1 |&1:12|
Other Form Products of JTT-851
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Recommended Products in the Same Indication
Chemical and Physical Properties
.Huang H, et al. Discovery of novel benzo[b]thiophene tetrazoles as non-carboxylate GPR40 agonists. Bioorg Med Chem Lett. 2017 Dec 12. pii: S0960-894X(17)31182-4.
GPR40 partial agonism is a promising new mechanism for the treatment of type 2 diabetes mellitus with clinical proof of concept. Most of the GPR40 agonists in the literature have a carboxylic acid functional group, which may pose a risk for idiosyncratic drug toxicity. A novel series of GPR40 agonists containing a tetrazole as a carboxylic acid bioisostere was identified. This series of compounds features a benzo[b]thiophene as the center ring, which is prone to oxidation during phase 1 metabolism. Following SAR optimization targeting GPR40 agonist activity and intrinsic clearance in microsomes (human and rat), potent and metabolically stable compounds were selected for in vivo evaluation. The compounds are efficacious at lowering blood glucose in a SD rat oGTT model.